S
Shiva Malek
Researcher at Genentech
Publications - 71
Citations - 5783
Shiva Malek is an academic researcher from Genentech. The author has contributed to research in topics: Lactate dehydrogenase & KRAS. The author has an hindex of 27, co-authored 67 publications receiving 4730 citations. Previous affiliations of Shiva Malek include University of California, San Diego & Exelixis.
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Journal ArticleDOI
RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
Georgia Hatzivassiliou,Kyung Song,Ivana Yen,Barbara J. Brandhuber,Daniel Anderson,Ryan Alvarado,Mary J. C. Ludlam,David Stokoe,Susan L. Gloor,Guy Vigers,Tony Morales,Ignacio Aliagas,Bonnie Liu,Steve Sideris,Klaus P. Hoeflich,Bijay S. Jaiswal,Somasekar Seshagiri,Hartmut Koeppen,Marcia Belvin,Lori Friedman,Shiva Malek +20 more
TL;DR: It is demonstrated that ATP-competitive kinase inhibitors can have opposing functions as inhibitors or activators of signalling pathways, depending on the cellular context, which provides new insights into the therapeutic use of ATP- competitive RAF inhibitors.
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Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity
Till Maurer,Lindsay S. Garrenton,Angela Oh,Keith Pitts,Daniel Anderson,Nicholas J. Skelton,Benjamin Fauber,Borlan Pan,Shiva Malek,David Stokoe,Mary J. C. Ludlam,Krista K. Bowman,Jiansheng Wu,Anthony M. Giannetti,Melissa A. Starovasnik,Ira Mellman,Peter K. Jackson,Joachim Rudolph,Weiru Wang,Guowei Fang +19 more
TL;DR: The discovery of a small-molecule binding pocket on Ras with functional significance provides a new direction in the search of therapeutically effective inhibitors of the Ras oncoprotein.
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The Crystal Structure of the IκBα/NF-κB Complex Reveals Mechanisms of NF-κB Inactivation
TL;DR: IkappaBalpha regulates the transcription factor NF-kappaB through the formation of stable Ikappa-Balpha/NF-KappaB complexes as discussed by the authors, which allows large en bloc movement of the p65 subunit amino-terminal domain.
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RAS-targeted therapies: is the undruggable drugged?
TL;DR: How drugs that target RAS or associated pathways might be used effectively, particularly in combinations, are explored, and other RAS-targeted therapies in the pipeline are discussed, including combination strategies.
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Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
Georgia Hatzivassiliou,Jacob R. Haling,Huifen Chen,Kyung Song,Steve Price,Robert Heald,Joanne Frances Mary Hewitt,Mark Zak,Ariana Peck,Ariana Peck,Christine Orr,Mark Merchant,Klaus P. Hoeflich,Jocelyn Chan,Shiuh-Ming Luoh,Daniel Anderson,Daniel Anderson,Mary J. C. Ludlam,Mary J. C. Ludlam,Christian Wiesmann,Christian Wiesmann,Mark Ultsch,Lori Friedman,Shiva Malek,Marcia Belvin +24 more
TL;DR: It is shown that, owing to distinct mechanisms regulating MEK activation in KRAS- versus BRAF-driven tumours, different mechanisms of inhibition are required for optimal antitumour activity in each genotype.